Erdman Vancomycin and Other Agents Learning Objectives

Question 1

Vanc MOA

Answer 1

Glycopeptide that inhibits sysnthesis of bacterial cell wall by blocking glycopeptide polymerization; inhibits synthesis and assembly during the second stage by binding to D-Ala-D-Ala portion = prevents cross-linking and further elongation

Question 2

Synercid MOA

Answer 2

Individually bind on the 50S ribosomal subunit to inhibit early and late stages of bacterial protein synthesis = bacteriostatic

Question 3

Oxazolidinones MOA

Answer 3

Bind to 50S ribosomal subunit near the surface interface of the 30S subunit = inhibits 70S initiation complex formation = inhibits protein synthesis = bacteriostatic

Question 4

Daptomycin MOA

Answer 4

Inserts lipophilic tail into cell wall to form a transmembrane channel = leakage of cellular contents and rapid depolarization

Question 5

Lipoglycopeptides MOA

Answer 5

Binds to D-Ala-D-Ala terminus = interferes with polymerization

Oritavancin and telavancin bind to membranes and insert lipophilic tail = cellular leakage of contents and rapid depolarization

Question 6

Vanc MOR

Answer 6

VRE, VRSA –> modification of D-Ala-D-Ala to D-Ala-D-lactate via van gene

VISA: thickening of peptidoglycan layer of cell wall

Question 7

Synercid MOR

Answer 7

Alteration of ribosomal binding site via erm gene

Question 8

Oxazolidinones MOR

Answer 8

Alteration of the ribosomal subunit target site

Question 9

Daptomycin MOR

Answer 9

Very rare

Question 10

Lipoglycopeptides MOR

Answer 10

Modification to D-Ala-D-Lactate

Question 11

Vanc spectrum of activity

Answer 11

Gram positive aerobic and anaerobic bacteria

PRSP, MSSA, MRSA, C. diff. (oral form okay for C. diff)

Question 12

Synercid spectrum of activity

Answer 12

PRSP, VRE (only faecium), MSSA, MRSA

Question 13

Oxazolidinones spectrum of activity

Answer 13

PRSP, VRE, MSSA, MRSA, VISA

Question 14

Daptomycin spectrum of activity

Answer 14

PRSP, VRE, MSSA, MRSA, VISA

Question 15

Lipoglycopeptides spectrum of activity

Answer 15

VRE, MSSA, MRSA, VISA, VRSA (oritavancin)

Question 16

Vanc major pharmacokinetic characteristics

Answer 16

Widely distributed (including adipose tissue)

Variable CSF penetration

Half-life progressively increases as renal function decreases

Not removed by hemodialysis

Question 17

Synercid major pharmacokinetic characteristics

Answer 17

Significant PAE

Hepatic/biliary excretion = no renal adjustment needed

Question 18

Oxazolidinones major pharmacokinetic characteristics

Answer 18

PAE

Oral bioavailability

Readily distributed to well-perfused tissues

Both renal and non-renal elimination = no renal adjustment

Question 19

Daptomycin major pharmacokinetic characteristics

Answer 19

Concentration dependent

Highly protein bound and distributes well into tissues

Renal elimination = requires renal dose adjustment

Question 20

Lipoglycopeptides major pharmacokinetic characteristics

Answer 20

Concentration dependent activity

Well distributed

Question 21

Telavancin and dialysis

Answer 21

kidney elimination = renal adjustment required

Question 22

Dalbavancin and dialysis

Answer 22

very loooooooooong half-life

renal adjustment required

Question 23

Oritavancin and dialysis

Answer 23

no renal adjustment

Question 24

Vanc clinical uses

Answer 24

MRSA, PRSP, C. diff (oral)

Question 25

Synercid clinical uses

Answer 25

VRE (faecium)

Question 26

Oxazolidinones clinical uses

Answer 26

VRE, nosocomial pneumonia, MRSA

Question 27

Daptomycin clinical uses

Answer 27

iUsed where vancomycin/linezolid cannot be used DO NOT USE FOR PNEUMONIA!!!

Question 28

Lipoglycopeptides clinical uses

Answer 28

Used where vancomycin, linezolid/tedizolid, and daptomycin cannot be used

Question 29

Vanc AE

Answer 29

Red man syndrome: infusion related NOT an allergic reaction Nephrotoxicity (reversible), ototoxicity (irreversible)

Question 30

Synercid AE

Answer 30

Venous irritation myalgias arthralgias

Question 31

Oxazolidinones AE

Answer 31

GI CNS Thrombocytopenia anemia

Question 32

Daptomycin AE

Answer 32

GI injection site reactions myopathy acute eosinophilic pneumonia

Question 33

Lipoglycopeptides AE

Answer 33

Red man syndrome (infusion related) Nephrotoxicity ***QTC prolongation Taste disturbance ***Pregnancy category C

Question 34

Synercid major interactions

Answer 34

Cytochrome P450 3A4 inhibitor 1. Statins 2. Cyclosporine 3. Tacrolimus 4. Carbamazepine

Question 35

Oxazolidinones major interactions

Answer 35

Monoamine oxidase inhibitors 1. Risk of serotonin syndrome if taking SSRI/SNRI

Question 36

Daptomycin major interactions

Answer 36

Statins --> increased myopathy

Question 37

Lipoglycopeptides major interactions

Answer 37

Telavancin/oritavancin = interfere with coagulation tests